Constrained analogues of procaine were synthesized, and their inhibiting activity against DNMT1 was tested. Among them, the most potent compound, derivative 3b, was also able to induce a recognizable demethylation of chromosomal satellite repeats in HL60 human myeloid leukemia cells and thus represents a lead compound for the development of a novel class of non-nucleoside DNMT1 inhibitors.
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http://hdl.handle.net/11386/1845456
Titolo: | Constrained analogues of procaine as novel small molecule inhibitors of DNA methyltransferase-1. |
Autori: | |
Data di pubblicazione: | 2008 |
Rivista: | |
Abstract: | Constrained analogues of procaine were synthesized, and their inhibiting activity against DNMT1 was tested. Among them, the most potent compound, derivative 3b, was also able to induce a recognizable demethylation of chromosomal satellite repeats in HL60 human myeloid leukemia cells and thus represents a lead compound for the development of a novel class of non-nucleoside DNMT1 inhibitors. |
Handle: | http://hdl.handle.net/11386/1845456 |
Appare nelle tipologie: | 1.1.2 Articolo su rivista con ISSN |
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